MA37763B1 - Difluoro-hexahydro-cyclopentaoxazinyl and difluoro-hexahydro-benzooxazinyls as bace1 inhibitors - Google Patents

Difluoro-hexahydro-cyclopentaoxazinyl and difluoro-hexahydro-benzooxazinyls as bace1 inhibitors

Info

Publication number
MA37763B1
MA37763B1 MA37763A MA37763A MA37763B1 MA 37763 B1 MA37763 B1 MA 37763B1 MA 37763 A MA37763 A MA 37763A MA 37763 A MA37763 A MA 37763A MA 37763 B1 MA37763 B1 MA 37763B1
Authority
MA
Morocco
Prior art keywords
hexahydro
difluoro
benzooxazinyls
cyclopentaoxazinyl
bace1 inhibitors
Prior art date
Application number
MA37763A
Other languages
French (fr)
Other versions
MA37763A1 (en
Inventor
Hans Hilpert
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of MA37763A1 publication Critical patent/MA37763A1/en
Publication of MA37763B1 publication Critical patent/MA37763B1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/536Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/041,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/121,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La présente invention concerne des difluorocyclopentaoxazinyles et des difluorobenzooxazinyles de formule (i), présentant une activité inhibitrice de bace1, leur préparation, des compositions pharmaceutiques les contenant et leur utilisation en tant que substances actives sur le plan thérapeutique. Les composés actifs de la présente invention sont utiles dans le traitement thérapeutique et/ou prophylactique de, par exemple, la maladie d'alzheimer.The present invention relates to difluorocyclopentaoxazinyls and difluorobenzooxazinyls of formula (i), having a bace1 inhibitory activity, their preparation, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and / or prophylactic treatment of, for example, Alzheimer's disease.

MA37763A 2012-06-26 2013-06-24 Difluoro-hexahydro-cyclopentaoxazinyl and difluoro-hexahydro-benzooxazinyls as bace1 inhibitors MA37763B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12173690 2012-06-26
PCT/EP2013/063086 WO2014001228A1 (en) 2012-06-26 2013-06-24 Difluoro-hexahydro-cyclopentaoxazinyls and difluoro-hexahydro-benzooxazinyls as bace1 inhibitors

Publications (2)

Publication Number Publication Date
MA37763A1 MA37763A1 (en) 2016-08-31
MA37763B1 true MA37763B1 (en) 2017-05-31

Family

ID=48672630

Family Applications (1)

Application Number Title Priority Date Filing Date
MA37763A MA37763B1 (en) 2012-06-26 2013-06-24 Difluoro-hexahydro-cyclopentaoxazinyl and difluoro-hexahydro-benzooxazinyls as bace1 inhibitors

Country Status (22)

Country Link
US (1) US9181232B2 (en)
EP (1) EP2864324B1 (en)
JP (1) JP6251257B2 (en)
KR (1) KR20150023450A (en)
CN (1) CN104470915B (en)
AU (1) AU2013283524B2 (en)
BR (1) BR112014029742A2 (en)
CA (1) CA2872181A1 (en)
CL (1) CL2014003325A1 (en)
CO (1) CO7151509A2 (en)
CR (1) CR20140528A (en)
EA (1) EA025273B1 (en)
HK (1) HK1206344A1 (en)
IL (1) IL236138A (en)
MA (1) MA37763B1 (en)
MX (1) MX2014014937A (en)
NZ (1) NZ702253A (en)
PE (1) PE20142450A1 (en)
PH (1) PH12014502623B1 (en)
SG (1) SG11201407576YA (en)
UA (1) UA113309C2 (en)
WO (1) WO2014001228A1 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ589590A (en) 2008-06-13 2012-05-25 Shionogi & Co Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity
AU2010328975B2 (en) 2009-12-11 2015-01-22 Shionogi & Co. Ltd. Oxazine derivative
US9540359B2 (en) 2012-10-24 2017-01-10 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity
TW201446758A (en) 2013-03-01 2014-12-16 Amgen Inc Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
KR20150124985A (en) 2013-03-08 2015-11-06 암젠 인크 Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
TW201623295A (en) 2014-04-11 2016-07-01 塩野義製藥股份有限公司 Dihydrothiazine and dihydrooxazine derivatives having BACE1 inhibitory activity
CN106795147B (en) 2014-08-08 2020-09-22 美国安进公司 Cyclopropyl fused thiazine-2-amine compounds as beta-secretase inhibitors and methods of use
WO2016150785A1 (en) 2015-03-20 2016-09-29 F. Hoffmann-La Roche Ag Bace1 inhibitors
US11629154B2 (en) 2018-04-27 2023-04-18 Shionogi & Co., Ltd. Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8703785B2 (en) 2008-10-22 2014-04-22 Shionogi & Co., Ltd. 2-aminopyrimidin-4-one and 2-aminopyridine derivatives both having BACE1-inhibiting activity
GB0912778D0 (en) * 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
AU2010328975B2 (en) * 2009-12-11 2015-01-22 Shionogi & Co. Ltd. Oxazine derivative
UA103272C2 (en) * 2009-12-11 2013-09-25 Ф. Хоффманн-Ля Рош Аг 2-amino-5,5-difluoro-5,6-dihydro-4h-[1,3]oxazines as bace1 and/or bace2 inhibitors

Also Published As

Publication number Publication date
AU2013283524B2 (en) 2017-03-30
CL2014003325A1 (en) 2015-04-24
WO2014001228A1 (en) 2014-01-03
EP2864324B1 (en) 2018-03-28
MA37763A1 (en) 2016-08-31
PH12014502623A1 (en) 2015-01-21
US9181232B2 (en) 2015-11-10
MX2014014937A (en) 2015-03-09
IL236138A0 (en) 2015-02-01
US20150133440A1 (en) 2015-05-14
EA201590066A1 (en) 2015-04-30
IL236138A (en) 2016-10-31
CR20140528A (en) 2015-01-12
CN104470915A (en) 2015-03-25
SG11201407576YA (en) 2015-03-30
CO7151509A2 (en) 2014-12-29
AU2013283524A1 (en) 2014-11-13
UA113309C2 (en) 2017-01-10
PH12014502623B1 (en) 2015-01-21
CA2872181A1 (en) 2014-01-03
HK1206344A1 (en) 2016-01-08
KR20150023450A (en) 2015-03-05
JP6251257B2 (en) 2017-12-20
CN104470915B (en) 2019-07-26
BR112014029742A2 (en) 2017-06-27
EP2864324A1 (en) 2015-04-29
NZ702253A (en) 2016-06-24
JP2015521640A (en) 2015-07-30
PE20142450A1 (en) 2015-01-28
EA025273B1 (en) 2016-12-30

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